Gastric-resistant isoniazid pellets reduced degradation of rifampicin in acidic medium

Isoniazid and rifampicin are considered the first-line medication for preventing and treating tuberculosis. Rifampicin is degraded in the stomach acidic environment, especially when combined with isoniazid, factor contributing to treatment failure. In this study, gastric-resistant isoniazid pellets were obtained to physical contact of this drug with rifampicin and to bypass the stomach´s acidic environment. The pellets were fabricated using the extrusion-spheronization technique. The coating process was conducted in a fluid spray coater using Acrycoat L 100(r) solution as the coating agent. The pellets obtained were submitted to a dissolution test in HCl 0.1 N and phosphate buffer media. The results indicated that optimum gastric-resistance was only attained with the highest amount of coating material, with isoniazid almost fully released in phosphate buffer. The amount of rifampicin released from its mixture with non-coated isoniazid pellets in HCl 0.1 N was less than that released from its mixture with the enteric-coated pellets. Acrycoat L 100(r) was shown to be an effective enteric/gastric-resistant coating since the stability of rifampicin appeared to be enhanced when physical contact of this drug with isoniazid was prevented at low pH.Isoniazida e rifampicina são fármacos de primeira escolha para a prevenção e tratamento da tuberculose. A rifampicina degrada-se em condições ácidas do estômago, principalmente na presença da isoniazida, o que contribui para a falha do tratamento. O presente trabalho teve como objetivo a obtenção de péletes de isoniazida gastrorresistentes, visando a evitar contato da rifampicina com isoniazida e consequente degradação no meio ácido estomacal. Os péletes foram produzidos pela técnica de extrusão-esferonização. O processo de revestimento foi conduzido em leito fluidizado com solução orgânica de Acrycoat L 100(r). Os péletes obtidos foram submetidos ao teste de dissolução em HCl 0,1 N e tampão fosfato. Os resultados indicam que a gastrorresistência foi obtida somente com a maior quantidade de revestimento, sendo a isoniazida liberada completamente no meio tampão fosfato. A quantidade de rifampicina dissolvida em meio ácido, quando associada a péletes de isoniazida não revestidos, foi menor do que a observada na presença de péletes de liberação entérica. O polímero Acrycoat L 100(r) mostrou-se eficiente para o recobrimento com a função de gastrorresistência, indicando que a instabilidade da rifampicina pode ser reduzida nas associações com a isoniazida através do revestimento entérico da isoniazida

Polymeric nanoparticles of Brazilian red propolis extract : preparation, characterization, antioxidant and leishmanicidal activity

The ever-increasing demand for natural products and biotechnology derived from bees and ultra-modernization of various analytical devices has facilitated the rational and planned development of biotechnology products with a focus on human health to treat chronic and neglected diseases. The aim of the present study was to prepare and characterize polymeric nanoparticles loaded with Brazilian red propolis extract and evaluate the cytotoxic activity of "multiple-constituent extract in co-delivery system" for antileishmanial therapies. The polymeric nanoparticles loaded with red propolis extract were prepared with a combination of poly-ε-caprolactone and pluronic using nanoprecipitation method and characterized by different analytical techniques, antioxidant and leishmanicidal assay. The red propolis nanoparticles in aqueous medium presented particle size (200–280 nm) in nanometric scale and zeta analysis (−20 to −26 mV) revealed stability of the nanoparticles without aggregation phenomenon during 1 month. After freeze-drying method using cryoprotectant (sodium starch glycolate), it was possible to observe particles with smooth and spherical shape and apparent size of 200 to 400 nm. Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) and thermal analysis revealed the encapsulation of the flavonoids from the red propolis extract into the polymeric matrix. Ultra performance liquid chromatography coupled with diode array detector (UPLC-DAD) identified the flavonoids liquiritigenin, pinobanksin, isoliquiritigenin, formononetin and biochanin A in ethanolic extract of propolis (EEP) and nanoparticles of red propolis extract (NRPE). The efficiency of encapsulation was determinate, and median values (75.0 %) were calculated using UPLC-DAD. 2,2-Diphenyl-1-picryhydrazyl method showed antioxidant activity to EEP and red propolis nanoparticles. Compared to negative control, EEP and NRPE exhibited leishmanicidal activity with an IC50 value of ≅38.0 μg/mL and 31.3 μg/mL, 47.2 μg/mL, 154.2μg/mL and 193.2 μg/mL for NRPE A1, NRPE A2, NRPE A3 and NRPE A4, respectively. Nanoparticles loaded with red propolis extract in co-delivery system and EEP presented cytotoxic activity on Leishmania (V.) braziliensis. Red propolis extract loaded in nanoparticles has shown to be potential candidates as intermediate products for preparation of various pharmaceutical dosage forms containing red propolis extract in the therapy against negligible diseases such as leishmaniasis

Traditional Uses, Chemical Constituents, and Biological Activities of Bixa orellana

Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent

Standardization of extracts from Momordica charantia L. (Cucurbitaceae) by total flavonoids content determination

La calidad de los extractos vegetales es influenciada por parámetros tales como el método de extracción, el líquido extractor, granulometría del material vegetal y proporción plantasolvente. La uniformidad de esos parámetros en la obtención de extractos es de gran importancia para garantizar la calidad de los mismos. El ensayo espectrofotométrico basado en la formación de complejos con el cloruro de aluminio fue aplicado en la dosificación de flavonoides de Momordica charantia L., lo cual evidenció diferencias significativas entre los métodos de extracción, líquidos extractores e proporciones planta-solvente. La solución extractiva que presentó el mayor tenor de flavonoides fue preparada por maceración, con etanol 70º GL, granulometría del material vegetal de hasta 710 µm y en la proporción planta-solvente 1,5:10.The quality of vegetable extracts is influenced by parameters such as: extraction method, extracting liquid, vegetable matter granulometry and plant:solvent ratio. The standardization of these parameters in obtaining extracts is of great importance in order to guarantee their quality. The spectrophotometric trial based on the formation of complexes with aluminum chloride was applied to evaluate the flavonoids contents of Momordica charantia L., which showed significant differences between the extraction methods, extracting liquids and plant:solvent ratios. The extractive solution which presented the greatest level of flavonoids was prepared by maceration, with ethanol 70º GL, vegetable matter granulometry up to 710 µm and plant:solvent ratio 1.5:10.La calidad de los extractos vegetales es influenciada por parámetros tales como el método de extracción, el líquido extractor, granulometría del material vegetal y proporción plantasolvente. La uniformidad de esos parámetros en la obtención de extractos es de gran importancia para garantizar la calidad de los mismos. El ensayo espectrofotométrico basado en la formación de complejos con el cloruro de aluminio fue aplicado en la dosificación de flavonoides de Momordica charantia L., lo cual evidenció diferencias significativas entre los métodos de extracción, líquidos extractores e proporciones planta-solvente. La solución extractiva que presentó el mayor tenor de flavonoides fue preparada por maceración, con etanol 70º GL, granulometría del material vegetal de hasta 710 ?m y en la proporción planta-solvente 1,5:10.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Standardization of extracts from Momordica charantia L. (Cucurbitaceae) by total flavonoids content determination

La calidad de los extractos vegetales es influenciada por parámetros tales como el método de extracción, el líquido extractor, granulometría del material vegetal y proporción plantasolvente. La uniformidad de esos parámetros en la obtención de extractos es de gran importancia para garantizar la calidad de los mismos. El ensayo espectrofotométrico basado en la formación de complejos con el cloruro de aluminio fue aplicado en la dosificación de flavonoides de Momordica charantia L., lo cual evidenció diferencias significativas entre los métodos de extracción, líquidos extractores e proporciones planta-solvente. La solución extractiva que presentó el mayor tenor de flavonoides fue preparada por maceración, con etanol 70º GL, granulometría del material vegetal de hasta 710 µm y en la proporción planta-solvente 1,5:10.The quality of vegetable extracts is influenced by parameters such as: extraction method, extracting liquid, vegetable matter granulometry and plant:solvent ratio. The standardization of these parameters in obtaining extracts is of great importance in order to guarantee their quality. The spectrophotometric trial based on the formation of complexes with aluminum chloride was applied to evaluate the flavonoids contents of Momordica charantia L., which showed significant differences between the extraction methods, extracting liquids and plant:solvent ratios. The extractive solution which presented the greatest level of flavonoids was prepared by maceration, with ethanol 70º GL, vegetable matter granulometry up to 710 µm and plant:solvent ratio 1.5:10.La calidad de los extractos vegetales es influenciada por parámetros tales como el método de extracción, el líquido extractor, granulometría del material vegetal y proporción plantasolvente. La uniformidad de esos parámetros en la obtención de extractos es de gran importancia para garantizar la calidad de los mismos. El ensayo espectrofotométrico basado en la formación de complejos con el cloruro de aluminio fue aplicado en la dosificación de flavonoides de Momordica charantia L., lo cual evidenció diferencias significativas entre los métodos de extracción, líquidos extractores e proporciones planta-solvente. La solución extractiva que presentó el mayor tenor de flavonoides fue preparada por maceración, con etanol 70º GL, granulometría del material vegetal de hasta 710 ?m y en la proporción planta-solvente 1,5:10.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Spray drying parameters optimization for chitosan microparticles as insulin carrier

O objetivo deste trabalho foi determinar a influência dos parâmetros de nebulização no rendimento, granulometria e morfologia das micropartículas de quitosana como potencial carreadores da insulina. Quitosana a 1% e 2% (m/v) foi nebulizada em diferentes condições de fluxo e temperatura de entrada. A granulometria foi estudada por microscopia óptica e a morfologia por MEV. A concentração de quitosana foi o fator que mais influenciou no rendimento. A forma esférica foi predominante, com distribuição granulométrica compatível para permanência no septo nasal. As soluções poliméricas mais concentradas e a inclusão de insulina levaram a um aumento no diâmetro das partículas e a uma superfície menos rugosa.This study aimed to determine the influence of spray drying parameters on yield, particle size distribution and morphology of chitosan microparticles with potential as insulin carrier. Chitosan 1% and 2% (w/v) solutions were spray dried under different flow rates and inlet temperatures. Particle size distribution was determined by optical microscopy and surface morphology was examined by SEM. Chitosan concentration was the major factor that influenced the yields. Spherical particles predominated and their granulometry distribution showed to be compatible with permanence in the nasal septum. Solutions with higher polymer content as well the addition of insulin led to an increase in particle size and a smoother surface.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Preformulation of a liquid dosage formulation of captopril for pediatric use: drug-excipient compatibility and stability studies

Currently, medications used in children are typically modified from pharmaceutical dosage forms designed for adults. Captopril is widely adapted to liquid formulations for use in hospitals. Its stability in the aqueous medium is reduced since it undergoes oxidation producing captopril disulfide (its main metabolite). The aim of this formulation study was to suggest favorable conditions for the development of a stable captopril formulation. The compatibility between the drug and excipients was evaluated by differential scanning calorimetry analysis (DSC). For studies in solution, different formulations were prepared according to a factorial design varying EDTA concentration, water purity and pH. The resultant formulations were stored at 60°C and analyzed over a twelve-day period using HPLC. The DSC curves obtained suggested, although not conclusive to elucidation, interactions of captopril with citric acid and sucralose. The stability study of these solutions revealed that the variables significantly influenced captopril content, which degraded at zero order kinetics and rates differing by a factor of up to 7 times, where pH proved the most influential factor. Interactions between variables were observed. Therefore, development of a stable captopril formulation is feasible provided EDTA and a buffering agent is used at suitable concentrations (0.08% and pH 3.85)

Gastric-resistant isoniazid pellets reduced degradation of rifampicin in acidic medium

Isoniazid and rifampicin are considered the first-line medication for preventing and treating tuberculosis. Rifampicin is degraded in the stomach acidic environment, especially when combined with isoniazid, factor contributing to treatment failure. In this study, gastric-resistant isoniazid pellets were obtained to physical contact of this drug with rifampicin and to bypass the stomach´s acidic environment. The pellets were fabricated using the extrusion-spheronization technique. The coating process was conducted in a fluid spray coater using Acrycoat L 100(r) solution as the coating agent. The pellets obtained were submitted to a dissolution test in HCl 0.1 N and phosphate buffer media. The results indicated that optimum gastric-resistance was only attained with the highest amount of coating material, with isoniazid almost fully released in phosphate buffer. The amount of rifampicin released from its mixture with non-coated isoniazid pellets in HCl 0.1 N was less than that released from its mixture with the enteric-coated pellets. Acrycoat L 100(r) was shown to be an effective enteric/gastric-resistant coating since the stability of rifampicin appeared to be enhanced when physical contact of this drug with isoniazid was prevented at low pH